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Defactinib

Chemical Structure : Defactinib

CAS No.: 1073154-85-4

Defactinib (VS-6063;VS6063;PF04554878;PF-04554878)

Catalog No.: PC-42951Not For Human Use, Lab Use Only.

Defactinib (VS-6063, PF-04554878) is a potent, selective and orally active FAK inhibitor, selectively inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Defactinib (VS-6063, PF-04554878) is a potent, selective and orally active FAK inhibitor, selectively inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines.
Defactinib shows no statistically significant changes in FAK phosphorylation at the other residues(Tyr 576/577, Tyr 925, or Tyr 861), also inhibits Pyk2 Tyr402 phosphorylation in HeyA8 cells.
Defactinib markedly decreases proliferation and increases apoptosis combined with paclitaxel, reduces levels of AKT and YB-1 in taxane-resistant cell lines.
Defactinib significantly reduces tumor growth, synergized with the mTOR inhibitor everolimus in xenograft models of pancreatic tumor.

Physicochemical Properties

M.Wt 510.4927
Formula C20H21F3N8O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 39 mg/mL

Chemical Name/SMILES

Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-

References

1. Kang Y, et al. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.

2. Shimizu T, et al. Cancer Chemother Pharmacol. 2016 May;77(5):997-1003.

3. Jones SF, et al. Invest New Drugs. 2015 Oct;33(5):1100-7.

4. François RA, et al. J Natl Cancer Inst. 2015 May 12;107(8). pii: djv123.

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